fulvestrant
An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.
Ligand Summary
UNII: 22X328QOC4
PubChem: 104741
Guide to Pharmacology: 1015
ChEMBL: CHEMBL1358
DrugCentral: 1255
LyCHI: D7416FK94ZF1
Target Activities
ESR1
Estrogen receptor
10 Activities
Items per page:
1 – 10 of 10
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.62 | J. Med. Chem., (2015) 58:12:4888 | ||||
IC50 | 8.22 | Bioorg. Med. Chem. Lett., (2000) 10:2:147 | ||||
IC50 | 8.31 | J. Med. Chem., (2007) 50:18:4471 | ||||
IC50 | 8.4 | J. Nat. Prod., (2009) 72:11:1944 | ||||
Ki | 8.98 | J. Med. Chem., (2003) 46:8:1408 | ||||
IC50 | 9.09 | J. Med. Chem., (2015) 58:20:8128 | ||||
EC50 | 9.4 | J. Med. Chem., (2015) 58:12:4888 | ||||
IC50 | 10.2 | J. Med. Chem., (2015) 58:20:8128 | ||||
Ki | 8.97999954 | |||||
Ki | 9.62 | ANTAGONIST | ||||
ESR2
Estrogen receptor beta
8 Activities
Items per page:
1 – 8 of 8
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.36 | J. Med. Chem., (2007) 50:18:4471 | ||||
IC50 | 7.68 | J. Med. Chem., (2015) 58:12:4888 | ||||
IC50 | 8.08 | Bioorg. Med. Chem. Lett., (2005) 15:17:3912 | ||||
IC50 | 8.15 | Bioorg. Med. Chem. Lett., (2000) 10:2:147 | ||||
IC50 | 8.42 | J. Nat. Prod., (2009) 72:11:1944 | ||||
Ki | 8.86 | J. Med. Chem., (2003) 46:8:1408 | ||||
Ki | 8.85999966 | |||||
Ki | 8.74 | ANTAGONIST | ||||
EPHX2
Bifunctional epoxide hydrolase 2
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.58 | Bioorg. Med. Chem. Lett., (2013) 23:13:3818 | ||||
IC50 | 8.22 | Bioorg. Med. Chem. Lett., (2013) 23:13:3818 | ||||
Ki | 7.59 | |||||
ESRRA
Steroid hormone receptor ERR1
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.7 | J. Med. Chem., (2013) 56:7:2779 | ||||
IC50 | 8.7 | |||||
PGR
Progesterone receptor
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.68 | J. Med. Chem., (2015) 58:20:8128 | ||||
GPER1
G-protein coupled estrogen receptor 1
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
- | 7 | |||||